专利号:WO-2024110994-A1 优先权日:2022-11-25 标题 :A process for the preparation of ledipasvir 发明人:GANGARAJULA SUDHAKAR; CHENNAM RAMU; KUMARAGURU THENKRISHNAN; BABURAO RODE HARIDAS; MADDI REDDY SRIDHAR; CHADA REDDY RAJI; GHOSH SUBHASH 权利人:COUNCIL OF SCIENT AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN OF S 摘要:The present disclosure relates to process for the preparation of Ledipasvir (I) or of its pharmaceutically acceptable salts. The present disclosure also provides novel intermediates (IV–XI) that are used in the synthesis of Ledipasvir. The main strategies of the present invention are late-stage functionalization such as difluorination and cyclopropanation of the key intermediates of Ledipasvir (I). (Formula (I))
专利号:US-8927739-B2 优先权日:2011-05-18 标 题 :Processes for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives 发明人:QIU YAO-LING; PENG XIAOWEN; KIM IN JONG; CAO HUI; TANG DATONG; OR YAT SUN; WANG GUOQIANG; XU GUOYOU 权利人:ENANTA PHARM INC 摘要:The present invention relates generally to an improved process for the preparation of 5-azaspiro[2.4]heptane-6-carboxylic acid and its derivatives which are useful intermediates in the synthesis of biologically active molecules, especially in the synthesis of hepatits C virus NS5A inhibitors. In particular, the present invention relates to processes and intermediates for the preparation of compounds of formulae (Ia), (Ib) and (Ic):
专利号:US-9718807-B2 优先权日:2012-06-05 标 题 :Synthesis of antiviral compound 发明人:SCOTT ROBERT WILLIAM; VITALE JUSTIN PHILIP; MATTHEWS KENNETH STANLEY; TERESK MARTIN GERALD; FORMELLA ALEXANDRA; EVANS JARED WAYNE 权利人:GILEAD PHARMASSET LLC 摘要:The present disclosure provides processes for the preparation of a compound of formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.
专利号:US-8921573-B2 优先权日:2011-10-18 标 题:Processes for the preparation of novel benzimidazole derivatives 发明人:TANG DATONG; XU GUOYOU; PENG XIAOWEN; YING LU; WANG CE; CAO HUI; LONG JIANG; KIM IN JONG; WANG GUOQIANG; QIU YAO-LING; OR YAT SUN 权利人:ENANTA PHARM INC 摘要:The present invention relates to processes and intermediates for the preparation of novel benzimidazole derivatives, especially in the synthesis of hepatitis C virus NS5A inhibitors. In particular, the present invention relates to processes and intermediates for the preparation of compounds of formulae (I-a):
专利号:US-10738028-B2 优先权日:2016-05-11 标题:Spiro three-membered ring, spiro five-membered ring peptide deformylase inhibitor and use thereof in antibacteria and anti-tumor 发明人:HU WENHAO; LV FENGPING; TANG YANG; LI ZIYAN; CHEN CHEN; WEI JIANHAI; DONG SUZHEN; QIAN YU 权利人:RUDONG RUIEN PHARMACEUTICAL TECH CO LTD 摘要:Disclosed are the anti-bacterial activity and the anti-tumor activity of a class of new spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, are effective against many antibiotic-resistant Gram-positive strains by inhibiting the activity of the peptide deformylase required in the synthesis of bacterial proteins, and do not affect the synthetic process of the main proteins of the human body, thus selectively killing bacteria. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, can affect the energy balance of the cancer cells through inhibiting the peptide deformylase of the mitochondria in the cells, so that the mitochondrial membrane is depolarized, ATP is exhausted and cell apoptosis is promoted, and has good inhibitory activities on many cancer cell strains such as colorectal cancer, leukemia, lung cancer, gastric cancer, cervical cancer, breast cancer, prostatic cancer, liver cancer and osteosarcoma at relatively lower concentrations. The structure of exemplary invention spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitors are represented by one or more of:
专利号:US-2013324740-A1 优先权日:2012-06-05 标题:Synthesis of antiviral compound